This invention relates to a composition for treating diarrhea, as well as to the use and to the preparation of said composition. Diarrhea is a widespread and recurring ailment that attacks adults, children, infants and warm-blooded animals throughout the world. It has been estimated that in the United States, 16.5 million children under the age of five years experience 21-37 million episodes of diarrhea each year, 10% of said episodes leading to a physician's visit. Over 200 thousand of the children are hospitalized and 325 to 425 of the children die, most of them infants under one year of age. On a worldwide basis, next to respiratory infections, diarrheal diseases are the leading cause of death among children under five years of age. Thus, it is evident that control of this condition deserves the attention of the medical and veterinary communities and is in need of an effective, low-cost, easily administrable therapeutic agent.
The proper relationship of nutrients, wastes, electrolytes, and water through the intestines depends on an appropriate balance of absorption and secretion of water and electrolytes by the intestinal epithelium. However, there are many forces that interfere with the normal functioning of the body, leading to diarrhea. These forces may involve infections, chemicals or radiation, for example, and may reflect the condition of the immune system, such as in HIV syndrome. The function of the anti-diarrheal agent generally is not to attack the cause of the condition, but to relieve the symptoms and discomfort associated with said condition.
The organisms responsible for diarrhea include those that cause amebiasis, cholera, infectious colitis, and bacteremia (particularly from Salmonella), in addition to the specific organisms, enterotoxigenic and invasive Escherichia coli, Giardia lamblia, Isospora belli, Shigella, Strongyloides stercoralis, and essentially all organisms for which there is effective antimicrobial therapy causing diarrhea in immuno-compromised hosts.
Other organisms guilty of producing diarrhea encompass viruses, such as cytomegalovirus, enteric adenovirus, picornavirus and rotavirus. Also, various parasites may be responsible for the condition. Included in this group, in addition to those already mentioned, are Entamoeba histolytica, cryptosporidium and Microsporidia species.
Some of the chemical agents causing diarrhea are adrenergic neuron blocking agents, such as reserpine and guanethidine; antimicrobials, such as sulfonamides, tetracyclines and most broad-spectrum agents; bile acids, carcinoid tumor secretions, e.g., 5-hydroxytryptamine and vasoactive intestinal peptide; cholinergic agonists and cholinesterase inhibitors; fatty acids; osmotic laxatives, such as sorbitol and saline cathartics; prokinetic agents, such as metoclopramide and domperidone; prostaglandins; quinidine; and stimulant laxatives.
Notwithstanding the above, in an article in Pediatric Anals 23:523-524 (October 1994), Dr. Robert A. Hoekelman, cautions that:
Non-antimicrobial medications should not be used for the treatment of diarrhea in infants and children because they provide no benefit and may worsen the diarrhea by slowing intestinal mobility and thereby the expulsion of organisms and toxins responsible for the diarrhea, and by preventing absorption and secretion from the intestinal wall. Some drugs that slow intestinal motility such as diphenoxylate hydrochloride-atropine sulfate and loperamide hydrochloride also may cause respiratory depression, coma, and death.